Damping of dopamine (DA) overactivity is an important principle in the treatment of various CNS-disorders such as schizophrenia and dyskinesia. This can be acheived by using postsynaptic DA-receptor blockers (neuroleptics) the use of which, however, is accompanied by several side-effects.
An alternative principle in order to inhibit DA function is to stimulate presynaptic DA-receptors (DA-autoreceptors) which inhibit DA-cell firing. This principle has been used with some success administering low doses of apomorphine to patients with schizophrenia and tardive dyskinesias. However, apomorphine has no selective action at DA autoreceptors since postsynaptic DA receptors are stimulated by slightly higher doses than those necessary for presynaptic DA receptors, leading to excitation.
Stimulation of central DA-receptors is also a well established treatment of Parkinson's disease.